Palbocent (Palbociclib) 125 MG – 21 Capsules

Description

Palbocent (Palbociclib)  is an inhibitor of cyclin-dependent kinases (CDK) 4 and 6. Cyclin D1 and CDK4/6 are downstream of signaling pathways which lead to cellular proliferation. It reduced cellular proliferation of estrogen receptor (ER)-positive breast cancer cell lines by blocking progression of the cell from G1 into S phase of the cell cycle. Treatment of breast cancer cell lines with the combination of Palbociclib and antiestrogens leads to decreased retinoblastoma (Rb) protein phosphorylation resulting in reduced E2F expression and signaling, and increased growth arrest compared to treatment with each drug alone.

In vitro treatment of ER-positive breast cancer cell lines with the combination of Palbociclib and antiestrogens led to increased cell senescence compared to each drug alone, which sustain for up to 6 days following Palbociclib removal and greater if antiestrogen treatment continue. In vivo studies using a patient-derived ER-positive breast cancer xenograft model demonstrated that the combination of Palbociclib and letrozole increased the inhibitionof Rb phosphorylation, downstream signaling, and tumor growth compared to each drug alone. Human bone marrow mononuclear cells treated with Palbociclib in the presence or absence of an anti-estrogen in vitro did not become senescent and resumed proliferation following Palbociclib withdrawal.

Use in Pregnancy & Lactation

Based on findings from animal studies and its mechanism of action, Palbociclib can cause fetal harm when administered to a pregnant woman. There are no available data in pregnant women to inform the drug-associated risk. In animal reproduction studies, the administration of Palbociclib to pregnant rats and rabbits during organogenesis resulted in embryo-fetal toxicity at maternal exposures that were ≥4 times the human clinical exposure based on AUC. Pregnant women should be advised about the potential risk to a fetus. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2%-4% and 15%-20%, respectively. There is no information regarding the presence in human milk, its effects on milk production, or the breastfed infant. Because of the potential for serious adverse reactions in breastfed infants from Palbociclib, advise a lactating woman not to breastfeed during treatment with Palbociclib and for 3 weeks after the last dose.

Pediatric Use: The safety and effectiveness in pediatric patients have not been established.

Geriatric Use: No overall differences in safety or effectiveness were observed between these patients and younger patients.

Hepatic Impairment: Mild hepatic impairment had no effect on the exposure of Palbociclib. The pharmacokinetics of Palbociclib has not been studied in patients with moderate or severe hepatic impairment.

Renal Impairment: 

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